Fused Heterocyclic Systems with s‐Triazine Ring. Part 2. Synthesis and Biological Activity of Fluorinated 2‐Amino‐4‐aryl‐3,4‐dihydro[1,3,5]triazino[1,2‐a]benzimidazoles.

Abstract

Triazine derivatives R 0655Fused Heterocyclic Systems with s-Triazine Ring. Part 2. Synthesis and Biological Activity of Fluorinated 2-Amino-4-aryl-3,4-dihydro[1,3,5]triazino[1,2-a]benzimidazoles. -New fluorinated triazinobenzimidazole derivatives (III) (7 examples) are synthesized via cyclocondensation of 2-guanidinobenzimidazole (I) with fluorinated aromatic aldehydes and screened for their antibacterial and bovine dihydrofolate reductase (DHFR) inhibitory activity. Some of them, e.g compound (IIId), are found to possess weak antibacterial activity, but none of these compounds significantly inhibits bovine DHFR. -(DOLZHENKO, A. V.; CHUI*, W.-K.; DOLZHENKO, A. V.; CHAN, L.-W.; J. Fluorine Chem. 126 (2005) 5, 759-763; Dep. Pharm., Natl. Univ. Singapore, Singapore 117543, Singapore; Eng.) -A. Forchert 39-149